78807-63-3

Upstream product

• 555-16-8 4-nitrobenzaldehdye 
• 3637-01-2 3,4-dimethylacetophenone 

Downstream Products

• 1234016-27-3 C₂₆H₂₂N₄O₂S 
• 1234016-34-2 C₂₆H₂₁ClN₄O₂S 
• 1232985-42-0 3-(3,4-dimethylphenyl)-5-(4-nitrophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide 
• 170643-56-8 3-(3,4-Dimethyl-phenyl)-5-(4-nitro-phenyl)-4,5-dihydro-1H-pyrazole 

Relevant academic research and scientific papers

Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives as EGFR TK inhibitors and potential anticancer agents

Fourty-two thiazolyl-pyrazoline derivatives were synthesized to screen for their EGFR kinase inhibitory activity. Compound 4-(4-chlorophenyl)-2-(3-(3,4- dimethylphenyl)-5-p-tolyl-4,5-dihydro-1H-pyrazol-1-yl)thiazole (11) displayed the most potent EGFR TK inhibitory activity with IC50 of 0.06 μM, which was comparable to the positive control. Molecular docking results indicated that compound 11 was nicely bound to the EGFR kinase. Compound 11 also showed significant antiproliferative activity against MCF-7 with IC 50 of 0.07 μM, which would be a potential anticancer agent.

Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents

Two series of pyrazole derivatives designing for potential EGFR kinase inhibitors have been discovered. Some of them exhibited significant EGFR inhibitory activity. Compound 3-(3,4-dimethylphenyl)-5-(4-methoxyphenyl)-4,5- dihydro-1H-pyrazole-1-carbothioamide (C5) displayed the most potent EGFR inhibitory activity with IC50 of 0.07 μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound C5 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the pyrazole derivatives own high antiproliferative activity against MCF-7. Compound C5 showed significant antiproliferative activity against MCF-7 with IC50 of 0.08 μM. Therefore, compound C5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.

SYNTHESIS, AND REACTIONS OF SOME NEW PYRAZOLINES FROM CHALCONES AND THE SCREENING OF THEIR ANTIBACTERIAL ACTIVITIES

Condensation of 4-methyl-2-methoxy-, 3,4-dimethyl- and/or 4-methyl-2-chloroacetophenone with p-chloro- and/or p-nitrobenzaldehyde gave the corresponding chalcones 1a-e.Condensation of 1 with hydrazine hydrate, phenylhydrazine, and/or semicarbazide gave the corresponding pyrazolines 2,9, and 10.Addition of formic, acetic and propionic acids to 2 yielded the corresponding derivatives 3,4 and 5.Addition of benzoyl chloride, benzenesulphonyl chloride and/or bromine to 2 yielded the corresponding derivatives 6,7 and 8.The antibacterial tests against Gram-positive, and Gram-negative bacteria, yeast, and fungi are also screened.